How does this medication work? What will it do for me?

Everolimus belongs to the class of medications called antineoplastics. It is used to treat certain forms of advanced cancers. It may be used in combination with other medications to treat certain types of advanced breast cancer. It may be used alone to treat pancreatic neuroendocrinetumours or PNET (tumours in the pancreas that produce chemical messengers) that have metastasized (spread) or progressed within the past year. Everolimus is also used to treat renal cell carcinoma (kidney cancer) that has spread, after other medications have been tried.

Everolimus has been granted a notice of compliance with conditions (NOC/c) by Health Canada. This means that Health Canada has approved this medication to be marketed based on promising evidence of effectiveness, but additional study results are needed to verify its effectiveness. An NOC/c is used to allow access to products that are used to treat or prevent serious, life-threatening, or severely debilitating illness.

Everolimus has conditional approval from Health Canada to be used for people with a condition called tuberous sclerosis complex. This approval is conditional, as research shows it may help reduce the growth of giant cell astrocytomas (SEGA, a type of brain tumour) in children over 3 years of age and angiomyolipomas (a type of non-cancerous kidney tumour) in adults over 18 years of age, however additional clinical trials still need to be completed.

Everolimus works by slowing the growth and spread of breast cancer cells, kidney cancer cells and pancreatic cells that produce hormones by blocking key enzymes. It may also reduce the size of brain and kidney tumours that occur with the genetic condition tuberous sclerosis complex.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

How should I use this medication?

The tablets for oral suspension are intended to be used to treat SEGA associated with TSC only. If you are using the tablets for oral suspension, the tablets must be mixed with water to prepare a suspension (particles of drug mixed into a liquid) before taking the medication. Use tap water or non-sparkling water only. Do not use juice or any other liquids. You may choose to use an oral syringe to mix the tablets and water, or mix the tablets with water in a small amount of water in a glass.

To use an oral syringe, place the prescribed number of everolimus tablets for suspension into the oral syringe. Draw 5 mL of water and 4 mL of air into the syringe. Let the syringe rest for 3 minutes, until the tablets have mixed with the water and formed a suspension. Gently invert the syringe 5 times immediately before taking the dose. After taking the dose, draw another 5 mL of water into the syringe and gently swirl the water in the syringe to wash any remaining medication off the sides of the syringe. Swallow the contents of the syringe.

To use a small glass, place the prescribed number of everolimus tablets for oral suspension into the glass containing approximately 25 mL of water and let the tablets and water stand for 3 minutes. Stir the contents gently with a spoon and drink the contents immediately. After taking the dose, add a small amount of water to the glass and gently swirl the contents of the glass or rinse any remaining medication off the sides of the glass. Swallow the contents of the glass.

These tablets for suspension should not be swallowed whole, broken or crushed. Once the suspension has been prepared, it should be taken immediately. If it is not administered within 60 minutes, safely discard the suspension and start over. Wash your hands before and after preparing the suspension.

Avoid drinking grapefruit juice or eating grapefruit, star fruit, or Seville oranges. These foods can slow down how the body gets rid of the medication and may result in too much medication in the body.

It is important that this medication be taken exactly as prescribed by your doctor. If you miss a dose, take it as soon as possible and continue with your regular schedule. If it is more than 6 hours after the time you normally take the medication, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature, protect it from light and moisture, and keep it out of the reach of children.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

Who should NOT take this medication?

Do not take everolimus if you:

are allergic to everolimus or any ingredients of the medication

are allergic to sirolimus or temsirolimus

What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

agitation

acne

changes to menstrual cycles

changes in sense of taste

constipation

cough

dehydration

diarrhea

difficulty sleeping

difficulty swallowing

dizziness

dry mouth

headache

loss of appetite

skin problems (e.g., rash, acne, dry skin, itchiness)

nausea

nail changes

unusual weakness or tiredness

vomiting

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not check with your doctor or seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Your doctor will do blood tests regularly to monitor the number of specific types of blood cells, including red blood cells, in your blood.

Bleeding: Everolimus may cause a reduced number of platelets in the blood, which can make it difficult to stop cuts from bleeding. If you have a medical condition or are taking medication that affects blood clotting, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

If you notice any signs of bleeding, such as frequent nosebleeds, unexplained bruising, vomiting coffee-ground like substances, or black and tarry stools, notify your doctor as soon as possible. Your doctor will order routine blood tests to make sure potential problems are caught early.

Clotting: This medication has been linked to clots in the leg and lungs. If you develop sudden pain with redness and swelling in one of your legs (usually in the calf), sudden difficulty breathing, or coughing up blood, contact your doctor immediately.

Breathing problems: This medication has been linked to inflammation and damage to the lungs. If you develop shortness of breath or a persistent cough, contact your doctor.

Cholesterol and triglycerides: This medication may cause an increase in the amount of cholesterol or triglycerides in the blood. If you have high cholesterol or are at risk for heart disease, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Diabetes: Everolimus may cause an increase in blood sugar levels and glucose tolerance may change.People with diabetes may find it necessary to monitor their blood sugar more frequently while using this medication.

If you have diabetes or are at risk for developing diabetes, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

If you experience signs of high blood sugar, such as increased thirst and urination, excessive hunger, unexplained weight loss or a fruity odour to your breath, contact your doctor as soon as possible.

Fertility: Everolimus can cause changes to sperm in men and may cause ovulation and menstrual bleeding to stop during treatment in women. These changes may continue after stopping the medication.

Fluid and electrolyte balance: This medication may cause the levels of electrolytes such as potassium, sodium, magnesium, chloride, and calcium in the blood to change while taking this medication. If you experience symptoms of fluid and electrolyte imbalance such as muscle pains or cramps; dry mouth; numb hands, feet, or lips; or racing heartbeat, contact your doctor as soon as possible. Your doctor will do blood tests regularly to monitor the levels of these electrolytes in your blood while you are taking this medication.

Grapefruit juice: Drinking grapefruit juice, or eating grapefruit, star fruit, or Seville oranges while you are taking everolimus can affect how the medication is removed from the body and may cause too much of the medication to build up in the body. This can cause possibly harmful side effects. You should avoid these foods while taking this medication.

Hepatitis B: There have been reports of flare-ups of hepatitis B occurring when people take everolimus. If you have a history of hepatitis B, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Infection: As well as killing tumour cells, everolimus can reduce the number of cells that fight infection in the body (white blood cells). If possible, avoid contact with people with contagious infections and public areas with lots of people. Tell your doctor immediately if you notice signs of an infection, such as fever or chills, severe diarrhea, shortness of breath, prolonged dizziness, headache, stiff neck, weight loss, or listlessness. Your doctor will do blood tests regularly to monitor the number of specific types of blood cells in your blood.

Kidney function: This medication can cause harm to the kidneys. While you are taking everolimus, your doctor should test your kidney function regularly with blood tests.

Liver function: Liver disease or reduced liver function may cause this medication to build up in the body, causing side effects. If you have liver problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. Your doctor may want to test your liver function regularly with blood tests while you are taking this medication.

If you experience symptoms of liver problems such as fatigue, feeling unwell, loss of appetite, nausea, yellowing of the skin or whites of the eyes, dark urine, pale stools, abdominal pain or swelling, and itchy skin, contact your doctor immediately.

Mouth ulcers: This medication commonly causes inflammation of the mucous membrane in your mouth resulting in mouth ulcers. Avoid using any alcohol, hydrogen peroxide, iodine, or thyme-containing mouthwashes as they can worsen the ulcers. Discuss proper treatment for mouth ulcers with your doctor.

Surgery: This medication causes changes to the blood and wound healing. Make sure anyone involved in your medical care knows you are taking everolimus.

Pregnancy: Everolimus may cause harm to an unborn baby. Women who may become pregnant while taking this medication must use an effective form of birth control, even if they have not had their first menstrual period. Effective birth control must be used during treatment with everolimus, and for at least eight weeks following the discontinuation of treatment. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: It is not known if everolimus passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

Children: Everolimus is not recommended for children with cancer who are less than 18 years of age. The safety and effectiveness of using this medication have not been studied for children with SEGA who are less than 1 year of age and there is limited information about the use of everolimus for children less than 3 years of age.

Seniors: People over 65 years of age are more likely to experience side effects while taking this medication. Your doctor may adjust your dose based on side effects and how well the medication is tolerated.

What other drugs could interact with this medication?

There may be an interaction between everolimus and any of the following:

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

stop taking one of the medications,

change one of the medications to another,

change how you are taking one or both of the medications, or

leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.